S80182 |
BYL719 |
源葉(MedMol) | 99% |
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- 產(chǎn)品描述: Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity
- 靶點: p110α:5 nM (IC50);p110β:1200 nM (IC50);p110δ:290 nM (IC50);p110γ:250 nM (IC50);p110α-H1047R:4 nM (IC50);p110α-E545K:4 nM (IC50);PI3K
- 體內(nèi)研究:
Alpelisib (BYL-719) (12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes and deposition of ectopic bone matrix. Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv)
- 參考文獻(xiàn):
1. Furet P, et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. 2. Fritsch C, et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther. 2014 May;13(5):1117-29. 3. Gobin B, et al. BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma. Int J Cancer. 2015 Feb 15;136(4):784-96.
- 溶解性: Soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.265 ml 11.326 ml 22.652 ml 5 mM 0.453 ml 2.265 ml 4.53 ml 10 mM 0.227 ml 1.133 ml 2.265 ml 50 mM 0.045 ml 0.227 ml 0.453 ml
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)